[CAS NO. 676596-65-9] 1-Azakenpaullone

Name: 1-Azakenpaullone
Brand: Arctom Scientific
SKU: SLK-S7193

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PRODUCTS SPECIFICATIONS [676596-65-9]

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Catalog

SLK-S7193

Brand

Selleck

CAS

676596-65-9

DESCRIPTION [676596-65-9]

Overview

MDL	MFCD09037522
Molecular Weight	328.16
Molecular Formula	C15 H10 Br N3 O
SMILES	BrC1=CC=C2C(C(CC(NC3=C4N=CC=C3)=O)=C4N2)=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	3.0473 mL	15.2365 mL	30.4729 mL
5 mM	0.6095 mL	3.0473 mL	6.0946 mL
10 mM	0.3047 mL	1.5236 mL	3.0473 mL
50 mM	0.0609 mL	0.3047 mL	0.6095 mL

Description

1-Azakenpaullone (1-Akp) is a potent and selective inhibitor with of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.

Targets

GSK-3α ^[1]	GSK-3β ^[1] (Cell-free assay)
	18 nM

In vitro

1-Azakenpaullone inhibits the CDK1/cyclin B, CDK5/p25, and GSK-3β effectively, with IC50 of 0.018 μM, 4.2 μM, and 2.0 μM, respectively. In human islets, 1-Azakenpaullone (5 mM) in combination with glucose (8 mM) stimulates the β-cell proliferation. 1-Azakenpaullone effectively stimulates INS-1E cells replication and protects INS-1E cells against glucolipotoxicity-induced cell death.

In vivo

Pretreatment with 1-Azakenpaullone (10 or 100 pmol, i.c.v.) attenuates the ketamine-induced locomotor hyperactivity, disruption of PPI and cognitive deﬁcits, and improves the ketamine-induced motor incoordination in rotarod test.

References

[1] Kunick C, et al. Bioorg Med Chem Lett. 2004, 14(2), 413-416.
[2] Liu H, et al. Diabetes. 2009, 58(3), 663-672.
[3] Stukenbrock H, et al. J Med Chem. 2008, 51(7), 2196-2207.
[4] Mussmann R, et al. J Biol Chem. 2007, 282(16), 12030-12037.
[5] Chan MH, et al. Schizophr Res. 2012, 136(1-3), 96-103.
[6] Leost M, et al. Eur J Biochem. 2000, 267(19), 5983-5994.